EA201300317A1 - DERIVATIVES OF QUINOLINE AND QUINOXALINE AS KINASE INHIBITORS - Google Patents
DERIVATIVES OF QUINOLINE AND QUINOXALINE AS KINASE INHIBITORSInfo
- Publication number
- EA201300317A1 EA201300317A1 EA201300317A EA201300317A EA201300317A1 EA 201300317 A1 EA201300317 A1 EA 201300317A1 EA 201300317 A EA201300317 A EA 201300317A EA 201300317 A EA201300317 A EA 201300317A EA 201300317 A1 EA201300317 A1 EA 201300317A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- quinoline
- quinoxaline
- derivatives
- kinase inhibitors
- pathological conditions
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Quinoline Compounds (AREA)
Abstract
В заявке описана группа производных хинолина и хиноксалина, содержащих фторированную этильную боковую цепь, которые являются селективными ингибиторами ферментов киназы PI3, и поэтому полезны для применения в медицине, например, для лечения воспалительных, аутоиммунных, сердечно-сосудистых, нейродегенеративных, метаболических, онкологических, ноцицептивных патологических состояний или патологических состояний глаз.The application describes a group of quinoline and quinoxaline derivatives containing a fluorinated ethyl side chain, which are selective inhibitors of PI3 kinase enzymes, and therefore are useful in medicine, for example, for the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive pathological conditions or pathological conditions of the eyes.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1014963.1A GB201014963D0 (en) | 2010-09-08 | 2010-09-08 | Therapeutic agents |
| GBGB1101128.5A GB201101128D0 (en) | 2011-01-21 | 2011-01-21 | Therapeutic agents |
| PCT/GB2011/051647 WO2012032334A1 (en) | 2010-09-08 | 2011-09-02 | Quinoline and quinoxaline derivatives as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201300317A1 true EA201300317A1 (en) | 2013-11-29 |
| EA024162B1 EA024162B1 (en) | 2016-08-31 |
Family
ID=45810169
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201300317A EA024162B1 (en) | 2010-09-08 | 2011-09-02 | Quinoline derivatives as kinase inhibitors |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US9029392B2 (en) |
| EP (1) | EP2614061B1 (en) |
| JP (1) | JP5820882B2 (en) |
| KR (1) | KR101880280B1 (en) |
| CN (1) | CN103153996B (en) |
| AR (1) | AR082799A1 (en) |
| AU (1) | AU2011300521B2 (en) |
| BR (1) | BR112013004750B1 (en) |
| CA (1) | CA2808959C (en) |
| CL (1) | CL2013000603A1 (en) |
| CO (1) | CO6680717A2 (en) |
| CY (1) | CY1116734T1 (en) |
| DK (1) | DK2614061T3 (en) |
| EA (1) | EA024162B1 (en) |
| ES (1) | ES2544289T3 (en) |
| HK (1) | HK1181754A1 (en) |
| HR (1) | HRP20150868T1 (en) |
| HU (1) | HUE025223T2 (en) |
| IL (1) | IL224841A (en) |
| MA (1) | MA34600B1 (en) |
| ME (1) | ME02203B (en) |
| MX (1) | MX2013002529A (en) |
| MY (1) | MY162396A (en) |
| NZ (1) | NZ607966A (en) |
| PL (1) | PL2614061T3 (en) |
| PT (1) | PT2614061E (en) |
| RS (1) | RS54202B1 (en) |
| SG (1) | SG187924A1 (en) |
| SI (1) | SI2614061T1 (en) |
| SM (1) | SMT201500195B (en) |
| TW (1) | TWI510489B (en) |
| WO (1) | WO2012032334A1 (en) |
| ZA (1) | ZA201301751B (en) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ587051A (en) | 2008-01-04 | 2012-12-21 | Intellikine Llc | Isoquinolinone derivatives, compositions and methods of inhibiting phosphatidyl inositol-3 kinase (pi3 kinase) |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| US8703778B2 (en) | 2008-09-26 | 2014-04-22 | Intellikine Llc | Heterocyclic kinase inhibitors |
| CA2760791C (en) | 2009-05-07 | 2017-06-20 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
| ES2593256T3 (en) | 2010-05-21 | 2016-12-07 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulations |
| AR082799A1 (en) * | 2010-09-08 | 2013-01-09 | Ucb Pharma Sa | DERIVATIVES OF QUINOLINE AND QUINOXALINE AS QUINASE INHIBITORS |
| WO2012064973A2 (en) | 2010-11-10 | 2012-05-18 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| CN103648499B (en) | 2011-01-10 | 2017-02-15 | 无限药品股份有限公司 | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
| CA2842190A1 (en) | 2011-07-19 | 2013-01-24 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
| EP2734520B1 (en) | 2011-07-19 | 2016-09-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2013032591A1 (en) | 2011-08-29 | 2013-03-07 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| ME03300B (en) | 2012-06-13 | 2019-07-20 | Incyte Holdings Corp | Substituted tricyclic compounds as fgfr inhibitors |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
| DK2986610T5 (en) | 2013-04-19 | 2018-12-10 | Incyte Holdings Corp | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CA2925944C (en) | 2013-10-04 | 2023-01-10 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CN104744435B (en) * | 2013-12-25 | 2017-03-01 | 上海医药工业研究院 | Quinolines, its salt, its intermediate, preparation method and application |
| EP4066834A1 (en) | 2014-03-19 | 2022-10-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders |
| WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (en) | 2015-02-20 | 2017-12-26 | Incyte Corp | BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS |
| EA038045B1 (en) | 2015-02-20 | 2021-06-28 | Инсайт Корпорейшн | Bicyclic heterocycles as fgfr inhibitors |
| GB201506786D0 (en) * | 2015-04-21 | 2015-06-03 | Ucb Biopharma Sprl | Therapeutic use |
| CN108349985A (en) | 2015-09-14 | 2018-07-31 | 无限药品股份有限公司 | Solid form, preparation method, the composition and its application method comprising it of isoquinolines |
| US10759806B2 (en) | 2016-03-17 | 2020-09-01 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors |
| GB201604970D0 (en) | 2016-03-23 | 2016-05-04 | Syngenta Participations Ag | Improvements in or relating to organic compounds |
| GB201608797D0 (en) * | 2016-05-19 | 2016-07-06 | Ucb Biopharma Sprl | Therapeutic use |
| US10919914B2 (en) | 2016-06-08 | 2021-02-16 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| WO2017223422A1 (en) | 2016-06-24 | 2017-12-28 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| CN108239076B (en) * | 2016-12-26 | 2021-07-06 | 中国医学科学院药物研究所 | Quinazoline compound, preparation method, application and pharmaceutical composition thereof |
| AR111960A1 (en) | 2017-05-26 | 2019-09-04 | Incyte Corp | CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION |
| GB201708856D0 (en) * | 2017-06-02 | 2017-07-19 | Ucb Biopharma Sprl | Seletalisib crystalline forms |
| EA202092649A1 (en) | 2018-05-04 | 2021-06-21 | Инсайт Корпорейшн | FGFR INHIBITOR SALTS |
| US11466004B2 (en) | 2018-05-04 | 2022-10-11 | Incyte Corporation | Solid forms of an FGFR inhibitor and processes for preparing the same |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| IL291901A (en) | 2019-10-14 | 2022-06-01 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| KR20220131900A (en) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Derivatives of FGFR inhibitors |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| AR126102A1 (en) | 2021-06-09 | 2023-09-13 | Incyte Corp | TRICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2009009968A (en) * | 2007-03-23 | 2009-10-08 | Amgen Inc | Heterocyclic compounds and their uses. |
| ES2446417T3 (en) | 2007-03-23 | 2014-03-07 | Amgen Inc. | 3-substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (PI3K) inhibitors |
| WO2008118454A2 (en) * | 2007-03-23 | 2008-10-02 | Amgen Inc. | Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer |
| EP2231641B1 (en) * | 2007-12-21 | 2016-06-01 | UCB Biopharma SPRL | Quinoxaline and quinoline derivatives as kinase inhibitors |
| GB0819593D0 (en) * | 2008-10-24 | 2008-12-03 | Ucb Pharma Sa | Therapeutic agents |
| WO2011058108A1 (en) * | 2009-11-12 | 2011-05-19 | Ucb Pharma S.A. | Quinoline and quinoxaline derivatives as kinase inhibitors |
| AR082799A1 (en) * | 2010-09-08 | 2013-01-09 | Ucb Pharma Sa | DERIVATIVES OF QUINOLINE AND QUINOXALINE AS QUINASE INHIBITORS |
-
2011
- 2011-08-30 AR ARP110103154A patent/AR082799A1/en active IP Right Grant
- 2011-09-02 CN CN201180049091.2A patent/CN103153996B/en active Active
- 2011-09-02 SI SI201130542T patent/SI2614061T1/en unknown
- 2011-09-02 MA MA35807A patent/MA34600B1/en unknown
- 2011-09-02 CA CA2808959A patent/CA2808959C/en active Active
- 2011-09-02 PT PT117554238T patent/PT2614061E/en unknown
- 2011-09-02 NZ NZ607966A patent/NZ607966A/en unknown
- 2011-09-02 ES ES11755423.8T patent/ES2544289T3/en active Active
- 2011-09-02 MX MX2013002529A patent/MX2013002529A/en active IP Right Grant
- 2011-09-02 DK DK11755423.8T patent/DK2614061T3/en active
- 2011-09-02 WO PCT/GB2011/051647 patent/WO2012032334A1/en active Application Filing
- 2011-09-02 JP JP2013527681A patent/JP5820882B2/en active Active
- 2011-09-02 RS RS20150538A patent/RS54202B1/en unknown
- 2011-09-02 EA EA201300317A patent/EA024162B1/en not_active IP Right Cessation
- 2011-09-02 MY MYPI2013000767A patent/MY162396A/en unknown
- 2011-09-02 BR BR112013004750-0A patent/BR112013004750B1/en active IP Right Grant
- 2011-09-02 HU HUE11755423A patent/HUE025223T2/en unknown
- 2011-09-02 PL PL11755423T patent/PL2614061T3/en unknown
- 2011-09-02 EP EP20110755423 patent/EP2614061B1/en active Active
- 2011-09-02 KR KR1020137008975A patent/KR101880280B1/en active IP Right Grant
- 2011-09-02 SG SG2013012794A patent/SG187924A1/en unknown
- 2011-09-02 ME MEP-2015-120A patent/ME02203B/en unknown
- 2011-09-02 AU AU2011300521A patent/AU2011300521B2/en active Active
- 2011-09-02 US US13/821,294 patent/US9029392B2/en active Active
- 2011-09-06 TW TW100132061A patent/TWI510489B/en active
-
2013
- 2013-02-21 IL IL224841A patent/IL224841A/en active IP Right Grant
- 2013-03-01 CL CL2013000603A patent/CL2013000603A1/en unknown
- 2013-03-07 ZA ZA2013/01751A patent/ZA201301751B/en unknown
- 2013-03-21 CO CO13056775A patent/CO6680717A2/en active IP Right Grant
- 2013-07-30 HK HK13108926.7A patent/HK1181754A1/en unknown
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2015
- 2015-08-11 SM SM201500195T patent/SMT201500195B/en unknown
- 2015-08-13 HR HRP20150868TT patent/HRP20150868T1/en unknown
- 2015-08-18 CY CY20151100718T patent/CY1116734T1/en unknown
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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| PC4A | Registration of transfer of a eurasian patent by assignment | ||
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